| 摘要 |
<p>NEW MATERIAL:A thyroliberine derivative and its salt of formula (PCA-His-Pro is pyroglutamyl-hystidylprolyl; X is OH or amino; m is 2-5; n is 1-2). EXAMPLE:epsilon-Thyroliberylaminocaproic acid. USE:An intermediate of a polymer having thyroliberine residue effective to accelerate the secretion of thyrotropic hormones. PROCESS:epsilon-Aminocaproic acid benzyl p-toluenesulfonic acid salt is reacted with N- benzyloxycarbonylproline in the presence of a water-soluble carbodiimide, and the reaction product is amidated simultaneously with the elimination of carboxyl-protecting group. The amino-protecting group of the resulting compound is eliminated by hydrogenation. The product is condensed, and hydrogenated to eliminate the amino-protecting group, to obtain the objective compound of formula wherein X is amine.</p> |
